17 results about "Dasatinib" patented technology

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The invention belongs to the field of biological medicine, and particularly relates to a nano-drug based on chondroitin sulfate as well as a preparation method and application of the nano-drug. Chondroitin sulfate (CS) and dasatinib (DAS) are connected through a GFLG connexon responded by cathepsin B (CTSB) to prepare the prodrug CS-GFLG-DAS (CGD), the prodrug CS-GFLG-DAS (CGD) is used for reversing the phenotype of cancer-related fibroblasts and reducing the biosynthesis of extracellular matrixes, fibrotic tumors are efficiently treated, and a new perspective is provided for optimizing the application of immunotherapy in fibrotic tumors.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a dalcotinib pharmaceutical composition and a preparation method thereof.The dalcotinib pharmaceutical composition is prepared from, by weight, 10-30 parts of dalcotinib, 25-60 parts of lactose, 25-60 parts of microcrystalline cellulose, 1-15 parts of carboxymethyl starch sodium and 0.5-5 parts of magnesium stearate; the average particle size D50 of the lactose is greater than or equal to 120 microns. The dalcotinib composition disclosed by the invention is high in dissolution rate, quick in disintegration, good in fluidity, capable of avoiding sticking, good in dissolution rate stability and simple in preparation process.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib vanillic acid crystal form and a preparation method thereof, and in the dasatinib vanillic acid crystal form provided by the invention, the molar ratio of dasatinib to vanillic acid to water is 1: 1: 1. The dasatinib vanillic acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.

Combination therapies for use in the treatment of brain tumours, particularly glioma and embryonal brain tumours. Disclosed herein are pharmaceutical compositions comprising a complex of Panobinostat and a cyclodextrin, a second pharmaceutical agent, and a pharmaceutically acceptable excipient, diluent or carrier, in which the second pharmaceutical agent is Niclosamide, Dasatinib or Duvelisib. Associated methods of treatment and use are further disclosed.

The application discloses a kind of synthesis method of dasatinib intermediate in the field of organic synthesis, with 2-aminothiazole-4-carboxylic acid as raw material, first and tert-pivaloyl chloride in situ generates mixed anhydride, further and 2-chloro-6-methylaniline condensation reaction occurs after, the compound 2 obtained is not separated directly hydrolyzed to obtain high-purity 2-amino-N-(2-chloro-6-methylphenyl) thiazole-5-formamide.Due to the mixed anhydride formed by tert-pivaloyl chloride has greater steric hindrance, and the further reaction of corresponding amine is conducive to the regioselectivity, and by-product tert-pivalic acid can be easily removed by post-treatment, so as to solve the disadvantages existing in the prior art, the unit operation involved in the whole preparation process is simpler, and the product purity and yield are higher, with good application prospect.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The present application relates to the m 6 Application of methylation level of A as glioma marker, the present application confirms the m 6 The methylation modification level is related to the prognosis condition of brain glioma, and the increase of methylation abundance and expression level means worse prognosis. In addition, the present application researches and confirms that the expression of lncRNA-WEE2-AS1 is related to the formation of drug resistance of anti-tumor drugs, and inhibiting the expression of the lncRNA helps to improve the resistance of dasatinib, and provides a feasible treatment scheme for the clinical targeted treatment of drug-resistant patients.

To provide an amorphous solid dispersion ("ASD") comprising dasatinib, a pharmaceutical composition comprising ASD, and a method of treatment comprising administration of the pharmaceutical composition.SOLUTION: Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions can be used in methods of treating a proliferative disorder, such as cancer, or in methods of delivering dasatinib to a patient regardless of whether the patient is concurrently using a gastric acid reducing agent or the patient has an elevated gastric pH. The composition may be particularly suitable for patients suffering from achlorhydria or hypoacidity, or Helicobacter pylori infection.SELECTED DRAWING: Figure 7

This invention belongs to the field of biotechnology and relates to the application of an inhibitor blocking the TRIB3 / SRC interaction, alone or in combination with an SRC kinase inhibitor, in the preparation of drugs for the prevention or treatment of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. Specifically, it discloses an inhibitor that overcomes resistance to traditional small molecule drugs and targets tumor migration and stemness by blocking the TRIB3 / SRC interaction, and its application, alone or in combination with an SRC kinase inhibitor, in the preparation of drugs for the prevention or treatment of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. The amino acid sequence of the TRIB3 / SRC kinase inhibitor is listed in SEQ ID No. 1, and the SRC kinase inhibitor is Dasatinib. We found that this peptide can promote the degradation of TRIB3 and SRC, inhibit tumor migration and stemness, and inhibit tumor development and progression. Combined use with an SRC kinase inhibitor shows significant efficacy, and therefore it is applied in the preparation of drugs for the treatment and prevention of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. The prepared drugs show significant efficacy in treating tumor diseases, with few toxic side effects and high safety, and have promising development prospects.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib fumaric acid crystal form and a preparation method thereof, and in the dasatinib fumaric acid crystal form provided by the invention, the molar ratio of dasatinib to fumaric acid to methanol is 1: 1: 1. The dasatinib fumaric acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.

The present invention relates to the prevention or mitigation of adverse effects related to gene therapy, such as the formation of anti-drug antibodies. Specifically, the invention relates to the prevention or mitigation of such side effects using a tyrosine kinase inhibitor such as dasatinib.

The present invention relates to a composition for inducing the reprogramming of type 1 alveolar cells into type 2 alveolar cells, comprising dasatinib as an active ingredient. According to the present invention, by reprogramming AT1 cells into AT2 cells using dasatinib, it is possible to efficiently secure AT2 cells, which were difficult to obtain in sufficient numbers. Furthermore, it is expected that cells with physiological activity similar to actual tissues can be secured by reprogramming AT1 cells into AT2 cells within the organoid while culturing the organoid itself, rather than culturing single cells.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib maleic acid crystal form and a preparation method thereof, and in the dasatinib maleic acid crystal form provided by the invention, the molar ratio of dasatinib to maleic acid to methanol is 1: 1: 1. The dasatinib maleic acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The application provides a combined drug for treating acute T lymphocyte leukemia and central nervous system leukemia and application thereof, and the combined drug for treating T-ALL comprises dasatinib and dabrafinib. The application creatively combines the drug dasatinib and the drug dabrafinib as a drug for treating T-ALL, and the combination has a significant synergistic effect, has a significant effect of inhibiting T-ALL cell proliferation than a single drug, has an effect of prolonging the survival time of a T-ALL mouse model, and relieves the progress of T-ALL combined with central nervous system leukemia. The application provides a new strategy and idea for treating acute T lymphocyte leukemia and acute T lymphocyte leukemia combined with central nervous system leukemia, and has a very significant meaning.